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Published on: October 21, 2010
Inhibitory Effect of 5-Aminoimidazole-4-Carbohydrazonamides Derivatives Against Candida spp. Biofilm on
C Gabriel1, L Grenho2,3,4,5,6,7, F Cerqueira1,8
1Health Sciences Faculty, University Fernando Pessoa, Porto, Portugal.
Abstract:
Candida can adhere and form biofilm on biomaterials commonly used in medical devices which is a key attribute that enhances its ability to cause infections in humans. Furthermore, biomaterial-related infections represent a major therapeutic challenge since Candida biofilms are implicated in antifungal therapies failure. The goals of the present work were to investigate the effect of three 5-aminoimidazole-4-carbohydrazonamides, namely (Z)-5-amino-1-methyl-N'-aryl-1H-imidazole-4-carbohydrazonamides [aryl = phenyl (1a), 4-fluorophenyl (1b), 3-fluorophenyl (1c)], on Candida albicans and Candida krusei biofilm on nanohydroxyapatite substrate, a well-known bioactive ceramic material. To address these goals, both quantitative methods (by cultivable cell numbers) and qualitative evaluation (by scanning electron microscopy) were used. Compounds cytocompatibility towards osteoblast-like cells was also evaluated after 24 h of exposure, through resazurin assay. The three tested compounds displayed a strong inhibitory effect on biofilm development of both Candida species as potent in vitro activity against C. albicans sessile cells. Regarding cytocompatibility, a concentration-dependent effect was observed. Together, these findings indicated that the potent activity of imidazole derivatives on Candida spp. biofilms on nanohydroxyapatite substrate, in particular compound 1c, is worth further investigating.
Insights
Three novel imidazole derivatives effectively inhibited Candida albicans and Candida krusei biofilm formation on nanohydroxyapatite. These compounds show promise for combating biomaterial-related fungal infections.
Area of Science:
- Medical Microbiology
- Materials Science
- Medicinal Chemistry
Background:
- Candida biofilms on biomaterials cause challenging human infections.
- Biofilm formation hinders effective antifungal therapies.
- Nanohydroxyapatite is a common bioactive ceramic in medical devices.
Purpose of the Study:
- To evaluate the anti-biofilm efficacy of three 5-aminoimidazole-4-carbohydrazonamide derivatives.
- To assess the impact of these compounds on Candida albicans and Candida krusei biofilms.
- To determine the cytocompatibility of the compounds with osteoblast-like cells.
Main Methods:
- Quantitative assessment of cultivable cell numbers.
- Qualitative evaluation using scanning electron microscopy.
- Resazurin assay for cytocompatibility testing.
Main Results:
- All three compounds significantly inhibited biofilm development in both Candida species.
- Potent in vitro activity against Candida albicans sessile cells was observed.
- Compound 1c demonstrated notable anti-biofilm effects and acceptable cytocompatibility.
Conclusions:
- Imidazole derivatives exhibit strong potential against Candida spp. biofilms on nanohydroxyapatite.
- Compound 1c warrants further investigation for therapeutic applications.
- These findings contribute to developing strategies against biomaterial-associated fungal infections.
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